PROTAC
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The PROTAC molecule itself contains three distinct portions: a ligand for binding to the target protein, a ligand for binding to an E3 ligase, and a linker joining these two ligands.
PROTACs (proteolysis-targeting chimaeras) are bifunctional molecules that bring a target protein into spatial proximity with an E3 ubiquitin ligase to trigger target ubiquitination and subsequent proteasomal degradation. Effective redirection of ligase poly-ubiquitination activity toward a new substrate protein requires formation of a ligase:PROTAC:target ternary complex, an intermediate species that is crucial to the cellular activity of degrader molecules. A characteristic feature of PROTACs mode of action is their sub-stoichiometric catalytic activity that alleviates the requirement for target engagement and occupancy of traditional inhibitors. New PROTAC molecules designed guided by the crystal structure show exquisite selectivity for inducing cellular depletion of Brd4 over its BET family members Brd2 and Brd3.
Products Related to PROTAC(273)
- GC80895PROTAC USP39 Degrader-1Purity: >98.00%
PROTAC USP39 Degrader-1 is a USP39 PROTAC degrader with K d values of 136 nM and 232 nM, and a DC 50 value of 1.06 nM (24 h).
- GC80896PROTAC D16-M1P2Purity: >98%
PROTAC D16-M1P2 is an orally active CRBN -mediated selective PKMYT1 PROTAC degrader, with a DC 50 of 0.7 nM in CCNE1-amplified HCC1569 breast cancer cells.
- GC80917LD-110 trihydrochloridePurity: >98.00%
LD-110 trihydrochloride is a highly efficient and effective LSD1 PROTAC degrader ( DC 50 = 0.44 μM).
- GC80920PROTAC PARP2 degrader-1CAS: 2925182-32-5Purity: >95.50%
PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC 50 of 2 μM.
- GC80922PROTAC HDAC6 degrader 7Purity: >98%
PROTAC HDAC6 degrader 7 is an orally active, highly efficient, and selective PROTAC degrader targeting histone deacetylase 6 ( HDAC6 ) ( IC 50 = 118 nM).
- GC80923PROTAC HDAC degrader-2 TFAPurity: >96.50%
PROTAC HDAC degrader-2 TFA is a selective class IIb dual histone deacetylase ( HDAC6 and HDAC10 ) PROTAC degrader, with DC 50 values of 13 nM and 29 nM against HDAC6 and HDAC10, respectively.
- GC80924iVeliparib-AP6CAS: 2472645-27-3Purity: >98%
iVeliparib-AP6 is a proteolysis-targeting chimera ( PROTAC ) molecule designed based on Veliparib, which targets PARP1/2.
- GC80934PROTAC BRD4 Degrader-49CAS: 3115940-40-1Purity: >98%
BRD4 degrader-8 is a BRD4 -targeting degrader.
- GC80936PROTAC BLIMP-1 degrader-1Purity: >98.00%
PROTAC BLIMP-1 degrader-1 is an orally active BLIMP-1 PROTAC degrader with an EC 50 of 13.1 nM.
- GC80937PROTAC KAT6 Degrader-1Purity: >98%
PROTAC KAT6 Degrader-1 is a CRBN-dependented KAT6 PROTAC degrader.
- GC80943KT-474 hydrochlorideCAS: 2751703-31-6Purity: >98.00%
KT-474 (KYM-001; PROTAC IRAK4 degrader-7) hydrochloride is an orally active PROTAC IRAK4 degrader with anti-tumor effects.
- GC80944PROTAC BCL6 Degrader-3CAS: 3005272-58-9Purity: >99.50%
PROTAC BCL6 Degrader-3 (compound 92) is a BCL6 PROTAC degrader.
- GC80945APH02174 hemiformicPurity: >98.00%
APH02174 hemiformic is a highly selective and orally active IRAK4 PROTAC degrader with the DC 50 of 4.01 nM in THP-1 cells.
- GC80946PROTAC JAK1/2 degrader-1Purity: >99.00%
PROTAC JAK1/2 degrader-1 is an orally active JAK1 / JAK2 PROTAC degrader, with DC 50 values of 1.4 μM and 0.92 μM against JAK1 and JAK2, respectively.
- GC80949PROTAC STAT6 degrader-3CAS: 3077385-98-6Purity: >98.00%
PROTAC STAT6 degrader-3 is a potent STAT6 PROTAC degrader with a DC 50 of less than 1 nM.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC80895 | PROTAC USP39 Degrader-1 | - | >98.00% | |
PROTAC USP39 Degrader-1 is a USP39 PROTAC degrader with K d values of 136 nM and 232 nM, and a DC 50 value of 1.06 nM (24 h). | ||||
| GC80896 | PROTAC D16-M1P2 | - | >98% | |
PROTAC D16-M1P2 is an orally active CRBN -mediated selective PKMYT1 PROTAC degrader, with a DC 50 of 0.7 nM in CCNE1-amplified HCC1569 breast cancer cells. | ||||
| GC80916 | ZX079 | 3124583-65-6 | >98% | |
ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC 50 value of 0.035 nM and a CBP DC 50 value of < 0.02 nM. | ||||
| GC80917 | LD-110 trihydrochloride | - | >98.00% | |
LD-110 trihydrochloride is a highly efficient and effective LSD1 PROTAC degrader ( DC 50 = 0.44 μM). | ||||
| GC80918 | dCBP-30 | - | >98% | |
dCBP-30 is an orally active, selective and dual-acting CBP/p300 PROTAC degrader with DC 50 values of 0.05 nM (CBP) and 0.04 nM (p300), respectively. | ||||
| GC80920 | PROTAC PARP2 degrader-1 | 2925182-32-5 | >95.50% | |
PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC 50 of 2 μM. | ||||
| GC80921 | CCT400028 | - | >98.00% | |
CCT400028 is a PROTACs -class degrader that targets the Aurora A (AURKA) kinase. | ||||
| GC80922 | PROTAC HDAC6 degrader 7 | - | >98% | |
PROTAC HDAC6 degrader 7 is an orally active, highly efficient, and selective PROTAC degrader targeting histone deacetylase 6 ( HDAC6 ) ( IC 50 = 118 nM). | ||||
| GC80923 | PROTAC HDAC degrader-2 TFA | - | >96.50% | |
PROTAC HDAC degrader-2 TFA is a selective class IIb dual histone deacetylase ( HDAC6 and HDAC10 ) PROTAC degrader, with DC 50 values of 13 nM and 29 nM against HDAC6 and HDAC10, respectively. | ||||
| GC80924 | iVeliparib-AP6 | 2472645-27-3 | >98% | |
iVeliparib-AP6 is a proteolysis-targeting chimera ( PROTAC ) molecule designed based on Veliparib, which targets PARP1/2. | ||||
| GC80928 | NP1192 | 2966791-41-1 | >99.00% | |
NP1192 is a potent, selective PROTAC NAT10 degrader. | ||||
| GC80934 | PROTAC BRD4 Degrader-49 | 3115940-40-1 | >98% | |
BRD4 degrader-8 is a BRD4 -targeting degrader. | ||||
| GC80935 | JQ1-JX5 | - | >98% | |
JQ1-JX5 is a DCAF16-based BRD4 PROTAC degrader. | ||||
| GC80936 | PROTAC BLIMP-1 degrader-1 | - | >98.00% | |
PROTAC BLIMP-1 degrader-1 is an orally active BLIMP-1 PROTAC degrader with an EC 50 of 13.1 nM. | ||||
| GC80937 | PROTAC KAT6 Degrader-1 | - | >98% | |
PROTAC KAT6 Degrader-1 is a CRBN-dependented KAT6 PROTAC degrader. | ||||
| GC80938 | DOT1L808 | - | >98.00% | |
DOT1L808 is a potent and highly selective DOT1L PROTAC degrader with a DC 50 value of 5 nM. | ||||
| GC80939 | MS115 TFA | 3109377-61-6 | >98.00% | |
MS115 TFA is a selective PRMT5/MEP50 PROTAC degrader, with DC 50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. | ||||
| GC80940 | dIRF4-2 | 3136609-62-3 | >99.00% | |
dIRF4-2 is a selective IRF4 PROTAC degrader with a DC 50 value of 2.2 μM. | ||||
| GC80941 | RJS308 TFA | - | >98.00% | |
RJS308 TFA is a selective Cyclophilin A ( CypA) PROTAC degrader. | ||||
| GC80943 | KT-474 hydrochloride | 2751703-31-6 | >98.00% | |
KT-474 (KYM-001; PROTAC IRAK4 degrader-7) hydrochloride is an orally active PROTAC IRAK4 degrader with anti-tumor effects. | ||||
| GC80944 | PROTAC BCL6 Degrader-3 | 3005272-58-9 | >99.50% | |
PROTAC BCL6 Degrader-3 (compound 92) is a BCL6 PROTAC degrader. | ||||
| GC80945 | APH02174 hemiformic | - | >98.00% | |
APH02174 hemiformic is a highly selective and orally active IRAK4 PROTAC degrader with the DC 50 of 4.01 nM in THP-1 cells. | ||||
| GC80946 | PROTAC JAK1/2 degrader-1 | - | >99.00% | |
PROTAC JAK1/2 degrader-1 is an orally active JAK1 / JAK2 PROTAC degrader, with DC 50 values of 1.4 μM and 0.92 μM against JAK1 and JAK2, respectively. | ||||
| GC80949 | PROTAC STAT6 degrader-3 | 3077385-98-6 | >98.00% | |
PROTAC STAT6 degrader-3 is a potent STAT6 PROTAC degrader with a DC 50 of less than 1 nM. | ||||